The purpose of this column is to highlight and summarize recent key patents in the pharmaceutical arena issued by the US Patent Office in June and July 2024.
Enhanced Penetration Ophthalmic Compositions of Bimatoprost Timodolol;
M. V. Shah, V. Subramanian, I. Subramanian, and A. Trehan; Somerset Therapeutics, USA; U.S. Patent # 12,042,502; July 23, 2024.
Glaucoma is a widespread, sight-threatening disease associated with elevated intraocular pressure (IOP), which can cause irreversible damage to the optic nerve and visual field. Management of glaucoma requires life-long treatment, typically by application of eye drops. The present invention contains a pharmaceutically acceptable and ophthalmologically suitable composition. It is in the form of a clear solution and contains a therapeutically effective amount of a bimatoprost compound and timolol compound, benzalkonium chloride, and a penetration enhancer component. The patent also provides a process for preparing these compositions and methods of their use in treating ocular conditions, such as methods of reducing elevated intraocular pressure and/or treating glaucoma, such as open-angle glaucoma.
Force Reduction in Injection Device;
M. Helmer, and S. Wendland; Sanofi, Paris, France; U.S. Patent # 12,048,836; July 30, 2024.
Auto-injector devices usually comprise a drive mechanism to expel a medicament. Depending on the properties of the medicament to be expelled, the force applied to the plunger by the drive should be varied. A high-impact force on the stopper can result in a negative user experience when using the injection device. The present application relates to force reduction in injection devices. The specification describes an injection device with a medicament container; a stopper translatable disposed within the medicament container; a plunger rod with a plunger head; a drive mechanism for displacing the plunger rod into the medicament container; and a force reduction feature. The plunger rod is operable to displace the stopper, and the force reduction feature is arranged to damp at least a part of a plunger rod motion.
Sustained Release Compositions of 4-Aminopyridine;
J.E. Cobb, Jr., T.B. Gold, R. D’Souza, and S. L. Way; Acorda Therapeutics, Inc., USA; U.S. Patent # 12,029,820; July 9, 2024.
The present invention generally relates to sustained-release 4-aminopyridine tablets, which include a core and a coating. The compressed core, comprises 4-aminopyridine, a polyethylene oxide with a molecular weight between 1,000,000 and 10,000,000, and a mixture comprising polyvinyl acetate and polyvinyl pyrrolidone. The coating surrounding the compressed core contains ethylcellulose. The ethylcellulose range is about 5% w/w to about 10% w/w of the compressed core. The tablets prepared provide a therapeutically effective amount of the active agent over 24 hours for the treatment of neurological disorders.
Injectable Preparation;
D. Kaneko, T. Matsuda, and Y. Hoshika; Otsuka Pharmaceutical Co., Tokyo, Japan; U.S. Patent # 12,016,927; June 25, 2024.
The present invention provides an injectable preparation that has a composition comprising a poorly soluble drug, a dispersion medium, and a specific suspending agent. The injectable preparation has excellent storage stability with no caking caused by precipitation of the particles of a poorly soluble drug. Because of stability, the preparation can be filled as is into a syringe to prepare prefilled syringes. This provides a compact lightweight medical instrument with reduced size and weight. The injectable preparation of the present invention becomes a gel upon standing, thus inhibiting precipitation and caking of the poorly soluble drug. It provides excellent storage stability. The preparation can be well dispersed intramuscularly or subcutaneously. With a mild impact, gel preparation gains fluidity (forms a sol state).
Formulation of Ear Drops and Methods for Delivery Thereof for Treating Upper Respiratory Infections;
S. Dhawan and Y. Dhawan; Maryland, USA and Lucknow, India; U.S. Patent # 12,029,814; July 9, 2024.
The patent describes a formulation and an uncommon route of administration to treat upper respiratory tract infections. This otic application includes at least one carrier medium and at least one antiviral agent. The formulation is designed in such a way as to transport the active agent across the tympanic membrane. The formulation contains – a mixture of jojoba oil and eucalyptus oil, and antiviral agents – hemin and remdesivir. Eucalyptus oil is added to the formulation as a means to detect if the formulation has reached the upper respiratory tract. The formulation can be added to the ear at room temperature or after warming slightly at about 40°C.
Liquid Delivery Composition;
F. Ferrari, C. Bonferoni, G. Sandri, L. M. Longo, C. Macelloni, and S. Rossi; Cosmo Technologies Ltd., Dublin, Irland; U. S. Patent # 12,011,483; June 18, 2024.
The patent describes a liquid composition comprising at least one thermo-responsive polymer (e.g., poloxamer), at least one ion[1]sensitive polymer (sodium alginate), and at least one bio-adhesive polymer (sodium carboxymethyl cellulose). Various types of drugs can be added to this base to produce a variety of liquids – solutions, suspensions, emulsions, syrups, etc. The liquid can be administered by injection with various routes of administration. The thermo-responsive polymer gels create a structured composition at the physiologic temperature. The ion-sensitive polymer gels when exposed to specific ions in the body. Both types of polymers, together, form a strong gel structure.
Treatment or Prevention Method of Radiation Damage by Administration of IL-5 Receptor Alpha Chain Binding Antibody;
K. Okada, K. Mori, S. Uematsu, and N. Takemura; Kyowa Kirin Co. Ltd. and The University of Tokyo, Tokyo, Japan; U.S. Patent # 11,999,788; June 4, 2024.
Radiotherapy is commonly used to treat cancers, which tend to damage normal cells/tissues. The damage is divided into two groups – early radiation damage, which occurs during radiation therapy, and delayed radiation damage, which develops several months to decades after the treatment. The invention describes a therapeutic or prophylactic agent for radiation damage, comprising an eosinophil-removing agent. It can be used with X-ray or gamma-ray radiation. The treatment can be applied to various kinds of cancers and various tissues. The active agent is an antibody or a fragment thereof that binds to the IL-5 receptor alpha chain or IL-5 ligand.
Author Details
Neelam Sharma, MS; Lakshmi Lavanya Kundurthy, BE; and Hemant N. Joshi, PhD, MBA*- Tara Innovations, LLC, www.tarainnovations.com *hemantjoshi.tara@gmail.com
Publication Details
This article appeared in American Pharmaceutical Review: Vol. 27, No. 6Sept/Oct 2024Pages: 94-95
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